CA3112043A1 - Polytherapies - Google Patents

Polytherapies Download PDF

Info

Publication number
CA3112043A1
CA3112043A1 CA3112043A CA3112043A CA3112043A1 CA 3112043 A1 CA3112043 A1 CA 3112043A1 CA 3112043 A CA3112043 A CA 3112043A CA 3112043 A CA3112043 A CA 3112043A CA 3112043 A1 CA3112043 A1 CA 3112043A1
Authority
CA
Canada
Prior art keywords
inhibitor
kras
formula
alkyl
optionally substituted
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
CA3112043A
Other languages
English (en)
Inventor
Lars Daniel ENGSTROM
Ruth Wei ARANDA
Peter Olson
James Gail Christensen
Jill HALLIN
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Mirati Therapeutics Inc
Original Assignee
Mirati Therapeutics Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Mirati Therapeutics Inc filed Critical Mirati Therapeutics Inc
Publication of CA3112043A1 publication Critical patent/CA3112043A1/fr
Pending legal-status Critical Current

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/2863—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against receptors for growth factors, growth regulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Immunology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Microbiology (AREA)
  • Mycology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

La présente invention concerne des polythérapies pour le traitement de cancers KRas G12C. En particulier, la présente invention concerne des méthodes de traitement du cancer chez un sujet en ayant besoin, comprenant l'administration au sujet d'une quantité thérapeutiquement efficace d'une combinaison d'un inhibiteur de la famille ErbB entière et d'un inhibiteur de KRAS G12C de formule (I), formule I-A ou formule I-B, des compositions pharmaceutiques comprenant une quantité thérapeutiquement efficace des inhibiteurs, des kits comprenant les compositions et des méthodes d'utilisation de ceux-ci.
CA3112043A 2018-09-10 2019-09-09 Polytherapies Pending CA3112043A1 (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862729189P 2018-09-10 2018-09-10
US62/729,189 2018-09-10
PCT/US2019/050227 WO2020055756A1 (fr) 2018-09-10 2019-09-09 Polythérapies

Publications (1)

Publication Number Publication Date
CA3112043A1 true CA3112043A1 (fr) 2020-03-19

Family

ID=69778045

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3112043A Pending CA3112043A1 (fr) 2018-09-10 2019-09-09 Polytherapies

Country Status (13)

Country Link
US (2) US12336995B2 (fr)
EP (1) EP3849538A4 (fr)
JP (2) JP7546548B2 (fr)
KR (1) KR102871791B1 (fr)
CN (1) CN112955137B (fr)
AU (1) AU2019340366B2 (fr)
CA (1) CA3112043A1 (fr)
EA (1) EA202190749A1 (fr)
IL (1) IL281344B2 (fr)
MX (2) MX2021002805A (fr)
SG (1) SG11202102377YA (fr)
WO (1) WO2020055756A1 (fr)
ZA (1) ZA202102015B (fr)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA3112043A1 (fr) * 2018-09-10 2020-03-19 Mirati Therapeutics, Inc. Polytherapies
CN114616232B (zh) * 2019-09-06 2026-05-05 正大天晴药业集团南京顺欣制药有限公司 氮杂环庚烷并嘧啶类衍生物及其医药用途
US12122787B2 (en) 2019-09-20 2024-10-22 Shanghai Jemincare Pharmaceuticals Co., Ltd Fused pyridone compound, and preparation method therefor and use thereof
CN112694475B (zh) * 2019-10-23 2025-09-23 苏州泽璟生物制药股份有限公司 环烷基类和杂环烷基类抑制剂及其制备方法和应用
WO2021085653A1 (fr) 2019-10-31 2021-05-06 Taiho Pharmaceutical Co., Ltd. Dérivés de 4-aminobut-2-enamide et sels de ces derniers
EP4067343A4 (fr) 2019-11-29 2024-01-03 Taiho Pharmaceutical Co., Ltd. Nouveau composé phénolique ou sel de celui-ci
US12702658B2 (en) 2020-04-24 2026-08-11 Taiho Pharmaceutical Co., Ltd. Anticancer combination therapy with N-(1-acryloyl-azetidin-3-yl)-2-((1H-indazol-3-yl)amino)methyl)-1H-imidazole-5-carboxamide inhibitor of KRAS-G12C
WO2021215544A1 (fr) 2020-04-24 2021-10-28 Taiho Pharmaceutical Co., Ltd. Inhibiteurs de protéine kras g12d
TW202144349A (zh) * 2020-04-30 2021-12-01 大陸商上海科州藥物研發有限公司 作為ｋｒａｓ抑制劑的雜環化合物的製備及其應用方法
WO2021260110A1 (fr) 2020-06-25 2021-12-30 Tolremo Therapeutics Ag Dérivés hétérocycliques, compositions pharmaceutiques et leur utilisation dans le traitement, le soulagement ou la prévention de maladie fibrotique
AU2021298154A1 (en) * 2020-06-25 2023-02-23 Tolremo Therapeutics Ag Combination of a CBP/p300 bromodomain inhibitor and a KRAS inhibitor for the treatment of cancer
WO2022109487A1 (fr) 2020-11-23 2022-05-27 Merck Sharp & Dohme Corp. Inhibiteurs 6,7-dihydro-pyrano[2,3-d]pyrimidine à substitution spirocyclique du mutant kras g12c
TWI895563B (zh) * 2020-12-08 2025-09-01 美商建南德克公司 用於治療實性瘤之包含ｋｒａｓｇ１２ｃ抑制劑及ｅｇｆｒ抑制劑之組成物及方法
US20240092803A1 (en) * 2021-01-08 2024-03-21 Beigene Switzerland Gmbh Bridged compounds as kras g12d inhibitor and degrader and the use thereof
CA3212085C (fr) 2021-04-07 2025-02-11 Tolremo Therapeutics Ag Dérives hétérocycliques, compositions pharmaceutiques et leur utilisation dans le traitement ou le soulagement du cancer
WO2023280026A1 (fr) * 2021-07-05 2023-01-12 四川科伦博泰生物医药股份有限公司 Composé cyclique hétéroaromatique, son procédé de préparation et son utilisation
KR20240051145A (ko) * 2021-07-29 2024-04-19 더 보드 오브 리젠츠 오브 더 유니버시티 오브 텍사스 시스템 Kras 돌연변이 암의 치료를 위한 방법 및 조성물
KR20240089340A (ko) 2021-10-05 2024-06-20 미라티 테라퓨틱스, 인크. 범 ErbB 계열 억제제와 KRAS G12D 억제제의 병용 요법
KR20240114793A (ko) 2021-11-05 2024-07-24 프론티어 메디슨즈 코포레이션 Kras g12c 억제제
US20230365595A1 (en) * 2022-05-13 2023-11-16 Ranok Therapeutics (Hangzhou) Co. Ltd. Inhibitors of kras(g12d)
KR20260096846A (ko) 2023-10-20 2026-06-24 머크 샤프 앤드 돔 엘엘씨 Kras 단백질의 소분자 억제제
CN122459678A (zh) 2023-12-29 2026-07-24 百时美施贵宝公司 KRAS抑制剂与Treg耗竭剂的组合疗法

Family Cites Families (296)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2417500C (fr) 2000-07-28 2008-11-18 Georgetown University Medical Center Inhibiteur de l'erbb-2 kinase selectif de petites molecules
CA2432578C (fr) 2001-01-02 2008-04-01 F. Hoffmann-La Roche Ag Derives quinazolone antagonistes de recepteur alpha 1a/b adrenergique
US7105667B2 (en) 2001-05-01 2006-09-12 Bristol-Myers Squibb Co. Fused heterocyclic compounds and use thereof
WO2002088079A2 (fr) 2001-05-01 2002-11-07 Bristol-Myers Squibb Company Inhibiteurs doubles de pde 7 et pde 4
JP2005522514A (ja) 2002-04-10 2005-07-28 ジェネンテック・インコーポレーテッド 抗ｈｅｒ２抗体改変体
CA2567832A1 (fr) 2004-06-04 2005-12-15 Astrazeneca Ab Derives de quinazoline utilises comme tyrosine kinases du recepteur erbb
UA90480C2 (uk) 2004-07-22 2010-05-11 Джэнэнтэк, Инк. Фармацевтична композиція, що має протипухлинну активність, яка включає антитіло до her2
US7812022B2 (en) 2004-12-21 2010-10-12 Glaxosmithkline Llc 2-pyrimidinyl pyrazolopyridine ErbB kinase inhibitors
AU2006236940A1 (en) 2005-04-14 2006-10-26 Wyeth Use of an epidermal growth factor receptor kinase inhibitor (EGFR) in gefitinib resistant patients
JP2009515878A (ja) 2005-11-12 2009-04-16 イーライ リリー アンド カンパニー 抗ｅｇｆｒ抗体
JP2009517451A (ja) 2005-12-02 2009-04-30 アストラゼネカ アクチボラグ Ｅｒｂｂチロシンキナーゼの阻害剤として使用されるキナゾリン誘導体
AR056857A1 (es) 2005-12-30 2007-10-24 U3 Pharma Ag Anticuerpos dirigidos hacia her-3 (receptor del factor de crecimiento epidérmico humano-3) y sus usos
US20080051387A1 (en) 2006-06-09 2008-02-28 Yuelian Xu Tetrahydropyrido[3,4-d]pyrimidines and related analogues
WO2008009078A2 (fr) 2006-07-20 2008-01-24 Gilead Sciences, Inc. Dérivés de la quinazoline tri-substitués en 4,6-dl et en 2,4,6 utilisables pour traiter les infections virales
EP2471816A1 (fr) 2006-08-30 2012-07-04 Genentech, Inc. Anticorps multi-spécifiques
AU2007296745B2 (en) 2006-09-11 2011-12-01 Curis, Inc. Quinazoline based EGFR inhibitors
CA2662617C (fr) 2006-09-11 2014-11-18 Changgeng Qian Inhibiteurs d'egfr a base de quinazoline contenant un fragment de liaison au zinc
US7547781B2 (en) 2006-09-11 2009-06-16 Curis, Inc. Quinazoline based EGFR inhibitors containing a zinc binding moiety
US8242080B2 (en) 2006-10-13 2012-08-14 The Regents Of The University Of California Inhibitors of the EGFR kinase targeting the asymmetric activating dimer interface
US20100210649A1 (en) 2006-12-21 2010-08-19 Sloan-Kettering Institute For Cancer Research Pyridazinones and furan-containing compounds
WO2008103470A2 (fr) 2007-02-21 2008-08-28 Trustees Of Columbia University In The City Of New York Composés létaux dépendants du signal de ras oncogénique
WO2009013305A1 (fr) 2007-07-24 2009-01-29 Novartis Ag Utilisation d'imidazoquinolines pour le traitement de maladies dépendant de egfr ou de maladies qui ont acquis une résistance à des agents qui ciblent des membres de la famille egfr
US8119616B2 (en) 2007-09-10 2012-02-21 Curis, Inc. Formulation of quinazoline based EGFR inhibitors containing a zinc binding moiety
ES2668831T3 (es) 2007-10-03 2018-05-22 Nippon Steel & Sumitomo Metal Corporation Aceros inoxidables austeníticos
WO2009047255A1 (fr) 2007-10-09 2009-04-16 Ucb Pharma, S.A. Composés hétérobicycliques utiles comme antagonistes du récepteur h4 de l'histamine
US8557243B2 (en) 2008-01-03 2013-10-15 The Scripps Research Institute EFGR antibodies comprising modular recognition domains
BRPI0908049A2 (pt) 2008-03-05 2015-08-11 Novartis Ag Uso de derivados de pririmidina para o tratamento de doenças dependentes de egfr ou de doenças que possuem resistência adquirida a agentes que são direcionados aos membros da família de egfr
US8163763B2 (en) 2008-07-31 2012-04-24 Genentech, Inc. Pyrimidine compounds, compositions and methods of use
US8642991B2 (en) 2008-11-11 2014-02-04 Samsung Electronics Co., Ltd. Photosensitive quantum dot, composition comprising the same and method of forming quantum dot-containing pattern using the composition
US20100143295A1 (en) 2008-12-05 2010-06-10 Auspex Pharmaceuticals, Inc. Quinazoline inhibitors of egfr tyrosine kinase
WO2010099186A1 (fr) 2009-02-25 2010-09-02 Merck Sharp & Dohme Corp. Compositions d'anticorps anti-her2
WO2010120996A1 (fr) 2009-04-17 2010-10-21 Wyeth Llc Composés de 5,6,7,8-tétrahydropyrido[3,4-d]pyrimidine, leur utilisation comme inhibiteurs de la mtor kinase et de la pi3 kinase, et leurs synthèses
AU2010239188B2 (en) 2009-04-22 2016-03-31 Janssen Pharmaceutica Nv Azetidinyl diamides as monoacylglycerol lipase inhibitors
KR101705158B1 (ko) 2009-05-05 2017-02-09 다나-파버 캔서 인스티튜트 인크. Ｅｇｆｒ 억제제 및 질환 치료방법
EP2510121A1 (fr) 2009-12-11 2012-10-17 Wyeth LLC Biomarqueurs de la voie de la phosphatidylinotisol-3-kinase
EP2513148B1 (fr) 2009-12-16 2016-08-31 AbbVie Biotherapeutics Inc. Anticorps anti-her2 et leurs utilisations
US20130029978A1 (en) 2009-12-25 2013-01-31 Mochida Pharmaceutical Co., Ltd. Novel aryl urea derivative
WO2011082285A1 (fr) 2009-12-30 2011-07-07 Avila Therapeutics, Inc. Modification covalente de protéine, dirigée sur un ligand
CN102167742B (zh) 2010-02-25 2014-05-14 上海百迈博制药有限公司 一种全人源抗her2单克隆抗体、其制备方法及用途
US20120107304A1 (en) 2010-04-27 2012-05-03 Boehringer Ingelheim International Gmbh Combination therapy in treatment of oncological and fibrotic diseases
WO2011140338A1 (fr) 2010-05-05 2011-11-10 Gatekeeper Pharmaceuticals, Inc. Composés modulant l'activité des récepteurs egfr et méthodes pour traiter ou prévenir des troubles à l'aide de ceux-ci
NZ604007A (en) 2010-05-27 2015-03-27 Genmab As Monoclonal antibodies against her2 epitope
US9051370B2 (en) 2010-08-10 2015-06-09 Glycotope Gmbh Humanized EGFR antibodies
ME02637B (fr) 2010-08-20 2017-06-20 Novartis Ag Anticorps pour le récepteur 3 du facteur de croissance épidermique (her3)
BR112013009624A2 (pt) 2010-11-08 2016-07-12 Novartis Ag uso de derivados de 2-carboxamida cicloamino ureia no tratamento de doenças dependemtes de egfr pu doenças que tenham adquirido resistência a agentes que tenham como alvo membros da família egfr
EP2637502B1 (fr) 2010-11-10 2018-01-10 Celgene CAR LLC Inhibiteurs d'egfr sélectifs d'un mutant et leurs utilisations
AU2012250517B2 (en) 2011-05-04 2016-05-19 Takeda Pharmaceutical Company Limited Compounds for inhibiting cell proliferation in EGFR-driven cancers
US8691231B2 (en) 2011-06-03 2014-04-08 Merrimack Pharmaceuticals, Inc. Methods of treatment of tumors expressing predominantly high affinity EGFR ligands or tumors expressing predominantly low affinity EGFR ligands with monoclonal and oligoclonal anti-EGFR antibodies
CN108424456B (zh) 2011-11-23 2022-04-26 医学免疫有限责任公司 特异于her3的结合分子及其用途
CN108341873B (zh) 2011-12-05 2022-03-25 诺华股份有限公司 表皮生长因子受体3(her3)的抗体
CN104203981A (zh) 2011-12-19 2014-12-10 合成免疫股份有限公司 双特异性抗体分子
US9034885B2 (en) 2012-01-13 2015-05-19 Acea Biosciences Inc. EGFR modulators and uses thereof
BR112014024131A2 (pt) 2012-03-29 2017-07-25 Shire Human Genetic Therapies lipídios catiônicos ionizáveis
WO2013155223A1 (fr) 2012-04-10 2013-10-17 The Regents Of The University Of California Compositions et méthodes pour le traitement du cancer
CN102659692B (zh) 2012-05-04 2014-04-09 郑州泰基鸿诺药物科技有限公司 双联厄洛替尼及其制备方法
JP6469567B2 (ja) 2012-05-05 2019-02-13 アリアド・ファーマシューティカルズ・インコーポレイテッド Ｅｇｆｒ発動性がんの細胞増殖阻害用化合物
CN106008511B (zh) 2012-05-14 2018-08-14 华东理工大学 蝶啶酮衍生物及其作为egfr、blk、flt3抑制剂的应用
TWI641619B (zh) 2012-06-25 2018-11-21 美商再生元醫藥公司 抗－ｅｇｆｒ抗體及其用途
US9695133B2 (en) 2012-07-13 2017-07-04 The Trustees Of Columbia University In The City Of New York Quinazolinone-based oncogenic-RAS-selective lethal compounds and their use
WO2014013019A1 (fr) 2012-07-18 2014-01-23 Glycotope Gmbh Nouveaux traitements thérapeutiques par anticorps anti-her2 à basse fucosylation
CN104755500B (zh) 2012-11-08 2020-10-02 霍夫曼-拉罗奇有限公司 结合HER3 β-发夹的HER3抗原结合蛋白
CN104755499B (zh) 2012-11-08 2020-10-02 霍夫曼-拉罗奇有限公司 结合HER3 β-发夹和HER4 β-发夹的抗HER3/HER4抗原结合蛋白
EP3181564B1 (fr) 2012-11-20 2019-09-18 H. Hoffnabb-La Roche Ag Composés d'aminopyrimidine comme inhibiteurs de mutants egfr de t790m
US20170275367A1 (en) 2012-11-21 2017-09-28 Janssen Biotech, Inc. Bispecific EGFR/C-Met Antibodies
KR102373193B1 (ko) 2012-11-21 2022-03-10 얀센 바이오테크 인코포레이티드 이중특이성 EGFR/c-Met 항체
CN103333246B (zh) 2012-12-21 2015-09-16 百奥泰生物科技(广州)有限公司 一种抗egfr受体的肿瘤生长抑制剂及其制备方法和用途
US10077672B2 (en) 2013-03-08 2018-09-18 United Technologies Corporation Ring-shaped compliant support
EP2970494B1 (fr) 2013-03-14 2017-12-13 The Board of Regents of The University of Texas System Anticorps monoclonaux spécifiques de her3 pour l'utilisation dans le diagnostic et thérapeutique
HK1219044A1 (zh) 2013-03-15 2017-03-24 艾伯维德国有限责任两合公司 抗egfr抗体药物偶联物制剂
WO2014143659A1 (fr) 2013-03-15 2014-09-18 Araxes Pharma Llc Inhibiteurs covalents irréversibles de la gtpase k-ras g12c
TW201524952A (zh) 2013-03-15 2015-07-01 Araxes Pharma Llc Ｋｒａｓ ｇ１２ｃ之共價抑制劑
US9227978B2 (en) 2013-03-15 2016-01-05 Araxes Pharma Llc Covalent inhibitors of Kras G12C
WO2014210354A1 (fr) 2013-06-28 2014-12-31 Genentech, Inc. Composés d'azaindazole en tant qu'inhibiteurs de la t790m contenant des mutants de l'egfr
TWI659021B (zh) 2013-10-10 2019-05-11 亞瑞克西斯製藥公司 Ｋｒａｓ ｇ１２ｃ之抑制劑
MX380928B (es) 2013-10-10 2025-03-12 Araxes Pharma Llc Inhibidores de kras g12c.
EP3092256B1 (fr) 2014-01-10 2022-05-18 Birdie Biopharmaceuticals Inc. Composés et compositions pour l'immunothérapie
NO2718543T3 (fr) 2014-02-04 2018-01-06
IL291000B2 (en) 2014-03-20 2024-04-01 Capella Therapeutics Inc Benzimidazole derivatives as erbb tyrosine kinase inhibitors for the treatment of cancer
CA2943231C (fr) 2014-03-20 2023-10-24 Capella Therapeutics, Inc. Derives de benzimidazole en tant qu'inhibiteurs de la tyrosine kinase erbb pour le traitement du cancer
TWI731535B (zh) 2014-03-21 2021-06-21 美商艾伯維有限公司 抗-egfr抗體及抗體藥物結合物
CA2943242A1 (fr) 2014-03-21 2015-09-24 X-Body, Inc. Polypeptides bi-specifiques de liaison a l'antigene
TWI871999B (zh) 2014-04-10 2025-02-01 日商第一三共股份有限公司 抗her3抗體-藥物結合物
EP3613433B1 (fr) 2014-05-30 2022-01-05 Shanghai Henlius Biotech, Inc. Anticorps du récepteur du facteur de croissance anti-épidermique (egfr)
EP3148981A4 (fr) 2014-05-30 2017-11-08 The Trustees of Columbia University in the City of New York Composés liant ras multivalents
AU2015271100B2 (en) 2014-06-06 2020-07-30 Redwood Bioscience, Inc. Anti-HER2 antibody-maytansine conjugates and methods of use thereof
CA2952834A1 (fr) 2014-06-20 2015-12-23 Abgenomics International Inc. Conjugues de medicaments-anticorps anti-her2
WO2016025650A1 (fr) 2014-08-13 2016-02-18 Celgene Avilomics Research, Inc. Combinaisons d'un inhibiteur de erk et d'un inhibiteur cdk4/6 et méthodes associées
SI3191135T1 (sl) 2014-09-12 2021-01-29 Genentech, Inc. Anti-HER2 protitelesa in imunokonjugati
CA2944085C (fr) 2014-09-16 2018-04-10 Ease Charm Limited Anticorps anti-egfr et leurs utilisations
JO3556B1 (ar) 2014-09-18 2020-07-05 Araxes Pharma Llc علاجات مدمجة لمعالجة السرطان
WO2016049565A1 (fr) 2014-09-25 2016-03-31 Araxes Pharma Llc Compositions et procédés pour inhiber la ras
US9862701B2 (en) 2014-09-25 2018-01-09 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
US10011600B2 (en) 2014-09-25 2018-07-03 Araxes Pharma Llc Methods and compositions for inhibition of Ras
EP3929190B1 (fr) 2014-10-13 2024-12-25 Yuhan Corporation Composés et compositions de modulation des activités de kinase mutant egfr
US20190209704A1 (en) 2014-10-20 2019-07-11 Igenica Biotherapeutics, Inc. Novel antibody-drug conjugates and related compounds, compositions and methods of use
US9862712B2 (en) 2014-11-20 2018-01-09 Council Of Scientific & Industrial Research Benzimidazole based EGFR inhibitors
AU2015360360B2 (en) 2014-12-11 2020-06-25 Beta Pharma (Shanghai) Co., Ltd. Substituted 2-anilinopyrimidine derivatives as EGFR modulators
WO2016105525A2 (fr) 2014-12-23 2016-06-30 Dana-Farber Cancer Institute, Inc. Nouvelles pyrimidines en tant qu'inhibiteurs d'egfr et procédés de traitement de troubles
CN104530063B (zh) 2015-01-13 2017-01-18 北京赛特明强医药科技有限公司 喹唑啉并杂环类化合物及其制备方法和作为用于治疗癌症的表皮生长因子受体抑制剂的应用
WO2016125186A1 (fr) 2015-02-03 2016-08-11 Council Of Scientific & Industrial Research Nouveaux inhibiteurs d'egfr à base de flavone et procédé de préparation associé
WO2016123706A1 (fr) 2015-02-03 2016-08-11 Trillium Therapeutics Inc. Nouveaux dérivés fluorés utilisés en tant qu'inhibiteurs d'egfr utiles pour le traitement de cancers
US10017540B2 (en) 2015-03-11 2018-07-10 California Institute Of Technology Cyclic peptide binder against oncogenic K-Ras
AU2016245864C1 (en) 2015-04-10 2021-09-09 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
ES2856880T3 (es) 2015-04-15 2021-09-28 Araxes Pharma Llc Inhibidores tricíclicos condensados de KRAS y métodos de uso de los mismos
WO2016172692A1 (fr) 2015-04-24 2016-10-27 H. Lee Moffitt Cancer Center And Research Institute, Inc. Inhibiteurs de kras mutant
AU2016258192B2 (en) 2015-05-06 2021-07-29 Leidos Biomedical Research, Inc. K-Ras modulators
EP3091033A1 (fr) 2015-05-06 2016-11-09 Gamamabs Pharma Anticorps anti-her3 humains et leurs utilisations
US10144724B2 (en) 2015-07-22 2018-12-04 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
HK1251624A1 (zh) 2015-09-24 2019-02-01 Ionis Pharmaceuticals, Inc. Kras表达的调节剂
US10730867B2 (en) 2015-09-28 2020-08-04 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
WO2017058902A1 (fr) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibiteurs de protéines mutantes kras g12c
WO2017058728A1 (fr) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibiteurs de protéines kras portant la mutation g12c
EP3356359B1 (fr) 2015-09-28 2021-10-20 Araxes Pharma LLC Inhibiteurs de protéines kras portant la mutation g12c
WO2017058768A1 (fr) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibiteurs de protéines kras portant la mutation g12c
EP3356347A1 (fr) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibiteurs de protéines kras portant la mutation g12c
US10975071B2 (en) 2015-09-28 2021-04-13 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
JP2018533939A (ja) 2015-10-19 2018-11-22 アラクセス ファーマ エルエルシー Ｒａｓの阻害剤をスクリーニングするための方法
US10670605B2 (en) 2015-10-22 2020-06-02 The Scripps Research Institute Cysteine reactive probes and uses thereof
WO2017080980A1 (fr) 2015-11-09 2017-05-18 Astrazeneca Ab Dérivés de dihydropyrrolopyrazinone utiles dans le traitement du cancer
WO2017079864A1 (fr) 2015-11-12 2017-05-18 Hangzhou Yier Biotech Co., Ltd. Traitement de cancers associés à un gène ras chroniquement actif
KR102932353B1 (ko) 2015-11-16 2026-02-27 아락세스 파마 엘엘씨 치환된 헤테로사이클릭 그룹을 포함하는 2-치환된 퀴나졸린 화합물 및 이의 사용 방법
WO2017100546A1 (fr) 2015-12-09 2017-06-15 Araxes Pharma Llc Procédés de préparation de dérivés de quinazoléine
US20170283445A1 (en) 2016-04-05 2017-10-05 University Of South Carolina Small Molecule Inhibitors Selective For Polo-Like Kinase Proteins
ES2863873T3 (es) * 2016-05-18 2021-10-11 Mirati Therapeutics Inc Inhibidores de KRAS G12C
CN109311858B (zh) 2016-05-26 2021-12-03 里科瑞尔姆Ip控股有限责任公司 Egfr抑制剂化合物
US10646488B2 (en) 2016-07-13 2020-05-12 Araxes Pharma Llc Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof
US10377833B2 (en) 2016-07-22 2019-08-13 Beijing Mabworks Biotech Co., Ltd. Bispecific anti-HER2 antibody
KR102469700B1 (ko) 2016-09-15 2022-11-23 우니베르지테트 스튜트가르트 Her3에 대한 항원 결합 단백질
JP2019529484A (ja) 2016-09-29 2019-10-17 アラクセス ファーマ エルエルシー Ｋｒａｓ ｇ１２ｃ変異体タンパク質の阻害剤
US10377743B2 (en) 2016-10-07 2019-08-13 Araxes Pharma Llc Inhibitors of RAS and methods of use thereof
MX2019006299A (es) 2016-11-30 2019-11-12 Bantam Pharmaceutical Llc Compuestos de pirazola sustituida y metodos para usarlos para el tratamiento de enfermedades hiperproliferativas.
JP2020513403A (ja) 2016-11-30 2020-05-14 バンタム、ファーマシューティカル、リミテッド、ライアビリティー、カンパニーＢａｎｔａｍ Ｐｈａｒｍａｃｅｕｔｉｃａｌ， Ｌｌｃ 置換ピラゾールおよびピロール化合物の使用する方法ならびに過剰増殖性疾患の治療のための方法
CN110291084A (zh) 2016-12-15 2019-09-27 加利福尼亚大学董事会 用于治疗癌症的组合物和方法
EP3558979B1 (fr) 2016-12-22 2021-02-17 Boehringer Ingelheim International GmbH Nouvelles quinazolines substituées benzylamino et dérivés en tant qu'inhibiteurs de sos1
CR20190338A (es) 2016-12-22 2019-09-09 Amgen Inc Inhibidores de kras g12c y métodos para su uso
US10344026B2 (en) 2017-01-18 2019-07-09 Nantbio, Inc. Compositions and methods of targeting mutant K-ras
EP3573954A1 (fr) 2017-01-26 2019-12-04 Araxes Pharma LLC Composés benzohétéroaromatiques bicycliques fusionnés et leurs procédés d'utilisation
US11136308B2 (en) 2017-01-26 2021-10-05 Araxes Pharma Llc Substituted quinazoline and quinazolinone compounds and methods of use thereof
EP3573971A1 (fr) 2017-01-26 2019-12-04 Araxes Pharma LLC Dérivés de 1-(3-(6-(3-hydroxynaphtalen-1-yl)benzofuran-2-yl)azétidin-1yl)prop-2-en-1-one et composés similaires utilisés en tant que modulateurs de kras g12c pour le traitement du cancer
JP7327802B2 (ja) 2017-01-26 2023-08-16 アラクセス ファーマ エルエルシー 縮合ヘテロ－ヘテロ二環式化合物およびその使用方法
WO2018140599A1 (fr) 2017-01-26 2018-08-02 Araxes Pharma Llc Composés à base de benzothiophène et de benzothiazole et leurs procédés d'utilisation
US20200385364A1 (en) 2017-01-26 2020-12-10 Araxes Pharma Llc Fused n-heterocyclic compounds and methods of use thereof
JOP20190186A1 (ar) 2017-02-02 2019-08-01 Astellas Pharma Inc مركب كينازولين
US11358940B2 (en) 2017-04-20 2022-06-14 The Regents Of The University Of California K-Ras modulators
US10640504B2 (en) 2017-09-08 2020-05-05 Amgen Inc. Inhibitors of KRAS G12C and methods of using the same
US10647715B2 (en) * 2017-11-15 2020-05-12 Mirati Therapeutics, Inc. KRas G12C inhibitors
CA3082579A1 (fr) 2017-11-15 2019-05-23 Mirati Therapeutics, Inc. Inhibiteurs de kras g12c
JP7058718B2 (ja) 2018-07-31 2022-04-22 本田技研工業株式会社 電力予測システム、電力予測装置、電力予測方法、プログラム、及び記憶媒体
SMT202500028T1 (it) * 2018-09-10 2025-03-12 Mirati Therapeutics Inc Terapie combinate
US12208099B2 (en) * 2018-09-10 2025-01-28 Mirati Therapeutics, Inc. Combination therapies
WO2020055755A1 (fr) * 2018-09-10 2020-03-19 Mirati Therapeutics, Inc. Polythérapies
CA3112043A1 (fr) * 2018-09-10 2020-03-19 Mirati Therapeutics, Inc. Polytherapies
AU2019338207B2 (en) * 2018-09-10 2025-01-02 Mirati Therapeutics, Inc. Combination therapies
CN109413550B (zh) 2018-09-30 2021-03-09 华为技术有限公司 音频播放电路和终端
CN111193490B (zh) 2018-11-14 2025-05-13 天津大学 散热结构、带散热结构的体声波谐振器、滤波器和电子设备
US12377101B2 (en) * 2018-12-05 2025-08-05 Mirati Therapeutics, Inc. Combination therapies
WO2020146613A1 (fr) 2019-01-10 2020-07-16 Mirati Therapeutics, Inc. Inhibiteurs de kras g12c
WO2020163598A1 (fr) 2019-02-07 2020-08-13 The Regents Of The University Of California Inhibiteurs dépendants d'immuophiline et leurs utilisations
EP3924687A4 (fr) 2019-02-11 2022-11-02 Mesomat Inc. Fibres de détection pour surveillance de contrainte structurelle
KR102747104B1 (ko) 2019-02-18 2024-12-27 한국과학기술연구원 단백질 키나아제 저해 활성을 갖는 신규한 피리도[3,4-d]피리미딘-8-온 유도체 및 이를 포함하는 암의 예방, 개선 또는 치료용 약학 조성물
GB2613715B (en) 2019-02-20 2023-12-06 Fred Hutchinson Cancer Center Binding proteins specific for RAS neoantigens and uses thereof
GB201902392D0 (en) 2019-02-21 2019-04-10 Cambridge Entpr Ltd Modular binding proteins
WO2020176693A2 (fr) 2019-02-26 2020-09-03 Cell Response, Inc. Procédés pour traiter des cancers positifs aux map3k8
WO2020177629A1 (fr) 2019-03-01 2020-09-10 劲方医药科技(上海)有限公司 Composé cyclique fusionné à une pyrimidine spiro-substitué, son procédé de préparation et son utilisation médicale
ES3010507T3 (en) 2019-03-05 2025-04-03 Astrazeneca Ab Fused tricyclic compounds useful as anticancer agents
US12117170B2 (en) 2019-03-05 2024-10-15 Questor Technology Inc. Gas incinerator system
EP3941938A1 (fr) 2019-03-06 2022-01-26 Dana-Farber Cancer Institute, Inc. Récepteurs de lymphocytes t spécifiques de l'antigène de maturation des lymphocytes b pour le traitement du cancer
WO2020198125A1 (fr) 2019-03-22 2020-10-01 Icahn School Of Medicine At Mount Sinai Procédés de traitement d'un cancer colorectal
WO2020205486A1 (fr) 2019-03-29 2020-10-08 Kura Oncology, Inc. Procédés de traitement de carcinomes squameux par des inhibiteurs de farnésyltransférase
WO2020205473A1 (fr) 2019-03-29 2020-10-08 Decerna Pharmaceuticals, Inc. Compositions et procédés pour le traitement de maladies et troubles associés au kras
KR102222693B1 (ko) 2019-04-04 2021-03-04 금정제약 주식회사 H-rev107 유래 펩타이드의 신규한 용도
WO2020214537A1 (fr) 2019-04-15 2020-10-22 Tosk, Inc. Modulateurs de ras gtpase
US20200335182A1 (en) 2019-04-16 2020-10-22 Uratim Ltd. Method and apparatus for facilitating the binding of biological macromolecules with the use of gluing molecular agents with applications in RAS mutations and related conditions
EP3964516A4 (fr) 2019-04-28 2023-01-11 Genfleet Therapeutics (Shanghai) Inc. Composé oxaazaquinazoline-7(8h)-cétone, son procédé de préparation et son application pharmaceutique
HRP20231310T1 (hr) 2019-05-10 2024-02-02 Deciphera Pharmaceuticals, Llc Heteroarilaminopirimidin amidni inhibitori autofagije i postupci njihove primjene
HUE065486T2 (hu) 2019-05-10 2024-05-28 Deciphera Pharmaceuticals Llc Fenilaminopirimidinamid autophágia inhibitorok és azok felhasználási eljárásai
EP4563150A3 (fr) 2019-05-13 2025-07-23 Novartis AG Nouvelles formes cristallines de n-(3-(2-(2-hydroxyéthoxy)-6-morpholinopyridin-4-yl)-4-méthylphényl-2(trifluorométhyl)isonicotinamide en tant qu'inhibiteurs de raf pour le traitement du cancer
EP3738593A1 (fr) 2019-05-14 2020-11-18 Amgen, Inc Dosage d'inhibiteur de kras pour le traitement de cancers
MY208668A (en) 2019-05-14 2025-05-23 Janssen Biotech Inc Combination therapies with bispecific anti-egfr/c-met antibodies and 3rd generation egfr tyrosine kinase inhibitors
CA3141604A1 (fr) 2019-05-20 2020-11-26 1200 Pharma Llc Inhibiteurs de kras g12c et leurs utilisations
US12252486B2 (en) 2019-05-21 2025-03-18 Amgen Inc. Solid state forms
EP3972973A1 (fr) 2019-05-21 2022-03-30 Amgen Inc. Formes à l'état solide
BR112021023136A2 (pt) 2019-05-21 2022-01-04 Inventisbio Co Ltd Compostos heterocíclicos, métodos de preparação e usos dos mesmos
WO2020234103A1 (fr) 2019-05-21 2020-11-26 Bayer Aktiengesellschaft Identification et utilisation d'inhibiteurs de kras
CA3142404A1 (fr) 2019-06-07 2020-12-10 Emory University Mutant g12v de kras se liant a jak1, inhibiteurs, compositions pharmaceutiques et procedes associes
US20220304984A1 (en) 2019-06-12 2022-09-29 Vanderbilt University Amino acid transport inhibitors and the uses thereof
WO2020252336A1 (fr) 2019-06-12 2020-12-17 Vanderbilt University Dibenzylamines utilisables comme inhibiteurs du transport des acides aminés
WO2021000885A1 (fr) 2019-07-01 2021-01-07 江苏恒瑞医药股份有限公司 Dérivés de quinazoline, leur procédé de préparation et leur utilisation médicale
IL290276B2 (en) 2019-08-02 2026-05-01 Shanghai Jemincare Pharmaceuticals Co Ltd Tetracyclic compounds, method for their preparation and use
US20210040089A1 (en) 2019-08-07 2021-02-11 Jacobio Pharmaceuticals Co., Ltd. Kras mutant protein inhibitors
CN114174298B (zh) 2019-08-14 2023-08-01 正大天晴药业集团南京顺欣制药有限公司 哒嗪酮并嘧啶类衍生物及其医药用途
CN112390797A (zh) 2019-08-15 2021-02-23 微境生物医药科技(上海)有限公司 新型螺环类K-Ras G12C抑制剂
CN114222743A (zh) 2019-08-16 2022-03-22 劲方医药科技(上海)有限公司 氧代六元环并嘧啶类化合物，其制法与医药上的用途
CN119454706A (zh) 2019-08-22 2025-02-18 密歇根大学董事会 治疗kras相关癌症的方法
CN114269735B (zh) 2019-08-26 2024-02-23 南京创济生物医药有限公司 二氢或四氢喹唑啉类化合物及其中间体、制备方法和应用
CN114615981B (zh) 2019-08-29 2024-04-12 米拉蒂治疗股份有限公司 Kras g12d抑制剂
JP2022554042A (ja) 2019-09-06 2022-12-28 ウェルマーカー・バイオ・カンパニー・リミテッド バイオマーカー型治療用組成物
CN114616232B (zh) 2019-09-06 2026-05-05 正大天晴药业集团南京顺欣制药有限公司 氮杂环庚烷并嘧啶类衍生物及其医药用途
US20220331401A1 (en) 2019-09-10 2022-10-20 The Board Of Trustees Of The Leland Stanford Junior University Methods of treating kras mutant cancers
TW202124374A (zh) 2019-09-13 2021-07-01 美商拜歐斯瑞克斯公司 Ras蛋白降解劑、其醫藥組合物及其治療應用
US20220402916A1 (en) 2019-09-18 2022-12-22 Merck Sharp & Dohme Corp. Small molecule inhibitors of kras g12c mutant
CN116947885B (zh) 2019-09-20 2026-01-23 上海济煜医药科技股份有限公司 稠合吡啶酮类化合物及其制备方法和应用
CN114502165A (zh) 2019-09-23 2022-05-13 苏州浦合医药科技有限公司 Shp2抑制剂及其用途
CN114761012B (zh) 2019-09-24 2025-03-21 米拉蒂治疗股份有限公司 组合疗法
US20210094919A1 (en) 2019-09-25 2021-04-01 Jacobio Pharmaceuticals Co., Ltd. Kras mutant protein inhibitors
CN114929706A (zh) 2019-09-29 2022-08-19 百济神州有限公司 Kras g12c的抑制剂
CN112574224A (zh) 2019-09-30 2021-03-30 上海迪诺医药科技有限公司 Kras g12c抑制剂及其应用
US20230257374A1 (en) 2019-10-10 2023-08-17 Innovent Biologics (Suzhou) Co., Ltd. Novel kras g12c protein inhibitor, preparation method therefor, and use thereof
JP6754125B1 (ja) 2019-10-15 2020-09-09 学校法人東京理科大学 Ｂｒａｐ２作用増強剤
US20240139193A1 (en) 2019-10-15 2024-05-02 Amgen Inc. Combination therapy of kras inhibitor and shp2 inhibitor for treatment of cancers
CN112694475B (zh) 2019-10-23 2025-09-23 苏州泽璟生物制药股份有限公司 环烷基类和杂环烷基类抑制剂及其制备方法和应用
WO2021080359A1 (fr) 2019-10-23 2021-04-29 에스케이바이오팜 주식회사 Composé bicyclique et son utilisation
AU2020369569B2 (en) 2019-10-24 2026-06-18 Amgen Inc. Pyridopyrimidine derivatives useful as KRAS G12C and KRAS G12D inhibitors in the treatment of cancer
MD4051678T2 (en) 2019-10-28 2026-07-31 Merck Sharp & Dohme Llc Small molecule inhibitors of the KRAS G12C mutant
BR112022008375A2 (pt) 2019-10-30 2022-07-12 Genfleet Therapeutics Shanghai Inc Composto cíclico heterocíclico fundido substituído, método de preparação e uso farmacêutico deste
WO2021084765A1 (fr) 2019-10-31 2021-05-06 Taiho Pharmaceutical Co., Ltd Dérivés de 4-aminobut-2-enamide et sels de ces derniers
WO2021085653A1 (fr) 2019-10-31 2021-05-06 Taiho Pharmaceutical Co., Ltd. Dérivés de 4-aminobut-2-enamide et sels de ces derniers
CN113286794B (zh) 2019-11-04 2024-03-12 北京加科思新药研发有限公司 Kras突变蛋白抑制剂
WO2021091956A1 (fr) 2019-11-04 2021-05-14 Revolution Medicines, Inc. Inhibiteurs de ras
CN121471132A (zh) 2019-11-04 2026-02-06 锐新医药公司 Ras抑制剂
MX2022005359A (es) 2019-11-04 2022-06-02 Revolution Medicines Inc Inhibidores de ras.
EP4043478A4 (fr) 2019-11-07 2024-01-03 Chugai Seiyaku Kabushiki Kaisha Composé peptidique cyclique ayant une action inhibitrice de kras
CN112778301A (zh) 2019-11-07 2021-05-11 苏州泽璟生物制药股份有限公司 四氢吡啶并嘧啶类抑制剂及其制备方法和应用
WO2021093758A1 (fr) 2019-11-15 2021-05-20 四川海思科制药有限公司 Dérivé de pyrimido et son application en médecine
CN114980976A (zh) 2019-11-27 2022-08-30 锐新医药公司 共价ras抑制剂及其用途
WO2021106231A1 (fr) 2019-11-29 2021-06-03 Taiho Pharmaceutical Co., Ltd. Composé ayant une activité inhibitrice contre la mutation kras g12d
WO2021104431A1 (fr) 2019-11-29 2021-06-03 苏州信诺维医药科技股份有限公司 Composé inhibiteur de kras g12c et son utilisation
EP4067343A4 (fr) 2019-11-29 2024-01-03 Taiho Pharmaceutical Co., Ltd. Nouveau composé phénolique ou sel de celui-ci
EP4015520B1 (fr) 2019-12-02 2025-02-19 280 Bio, Inc. Composé hétérocyclique contenant de l'oxygène, son procédé de préparation et son utilisation
WO2021113595A1 (fr) 2019-12-06 2021-06-10 Beta Pharma, Inc. Dérivés de phosphore utilisés comme inhibiteurs de kras
WO2021120045A1 (fr) 2019-12-18 2021-06-24 InventisBio Co., Ltd. Composés hétérocycliques, leurs procédés de préparation et utilisations associées
WO2021126799A1 (fr) 2019-12-18 2021-06-24 Merck Sharp & Dohme Corp. Peptides macrocycliques en tant qu'inhibiteurs puissants du mutant g12d de la k-ras
WO2021121397A1 (fr) 2019-12-19 2021-06-24 首药控股(北京)股份有限公司 Composé hétérocyclique alcynyle substitué
CA3165238A1 (fr) 2019-12-19 2021-06-24 Jacobio Pharmaceuticals Co., Ltd. Inhibiteurs de proteine mutante kras
CN114761408B (zh) 2019-12-19 2023-09-15 贝达药业股份有限公司 Kras g12c抑制剂及其在医药上的应用
TR201920922A2 (tr) 2019-12-20 2020-06-22 Ankara Ueniversitesi 3/4-((2E,6E)-3,7,11-Trimetildodeka-2,6,10-trieniltiyo)benzamid Türevi Bileşikler
CA3164995A1 (fr) 2019-12-20 2021-06-24 Erasca, Inc. Pyridones et pyrimidones tricycliques
AU2020414943A1 (en) 2019-12-27 2022-08-04 Wigen Biomedicine Technology (shanghai) Co., Ltd. Spiro ring-containing quinazoline compound
CN113045565A (zh) 2019-12-27 2021-06-29 微境生物医药科技(上海)有限公司 新型K-Ras G12C抑制剂
WO2021139678A1 (fr) 2020-01-07 2021-07-15 广州百霆医药科技有限公司 Inhibiteur pyridopyrimidine de protéine mutante kras g12c
WO2021139748A1 (fr) 2020-01-08 2021-07-15 Ascentage Pharma (Suzhou) Co., Ltd. Tétrahydroquinazolines spirocycliques
WO2021142252A1 (fr) 2020-01-10 2021-07-15 Incyte Corporation Composés tricycliques en tant qu'inhibiteurs de kras
EP4092026A4 (fr) 2020-01-13 2024-03-06 Suzhou Zelgen Biopharmaceutical Co., Ltd. Dérivé de pyridone ou de pyrimidine aryle ou hétéroaryle, son procédé de préparation et son utilisation
KR102396930B1 (ko) 2020-01-15 2022-05-12 한국과학기술연구원 피리도[3,4-d]피리미딘 유도체 및 이를 포함하는 치료용 약학 조성물
KR102382613B1 (ko) 2020-01-15 2022-04-06 한국과학기술연구원 단백질 키나아제 저해 활성을 갖는 7-아미노-3,4-디히드로피리미도피리미딘-2-온 유도체 및 이를 포함하는 치료용 약학 조성물
WO2021150613A1 (fr) 2020-01-20 2021-07-29 Incyte Corporation Composés spiro en tant qu'inhibiteurs de kras
WO2021147967A1 (fr) 2020-01-21 2021-07-29 南京明德新药研发有限公司 Composé macrocyclique servant d'inhibiteur de kras
GB202001344D0 (en) 2020-01-31 2020-03-18 Redx Pharma Plc Ras Inhibitors
US20230099858A1 (en) 2020-02-20 2023-03-30 Beta Pharma, Inc. Pyridopyrimidine derivatives as kras inhibitors
EP4112606A4 (fr) 2020-02-24 2024-04-10 Shanghai Zheye Biotechnology Co., Ltd. Composé aromatique et son utilisation dans la préparation de médicaments antinéoplasiques
TW202140450A (zh) 2020-02-24 2021-11-01 大陸商泰勵生物科技（上海）有限公司 用於癌症治療的ｋｒａｓ抑制劑
WO2021173923A1 (fr) 2020-02-28 2021-09-02 Erasca, Inc. Hétérocycles fusionnés à la pyrrolidine
CN114901663B (zh) 2020-03-02 2024-07-02 上海喆邺生物科技有限公司 一类芳香杂环类化合物及其在药物中的应用
US20230099204A1 (en) 2020-03-03 2023-03-30 Wellmarker Bio Co., Ltd. Pharmaceutical composition for prevention or treatment of cancer in which kras mutation and activated ron are present
IL296091A (en) 2020-03-05 2022-11-01 Univ Michigan Regents Inhibitors of braf, kras, egfr and other targets and their uses
CN115397413A (zh) 2020-03-05 2022-11-25 密歇根大学董事会 Egfr、kras、braf和其他靶标的抑制剂及其用途
CN115298174B (zh) 2020-03-12 2023-11-03 德昇济医药(无锡)有限公司 嘧啶并杂环类化合物及其应用
TW202144345A (zh) 2020-03-17 2021-12-01 大陸商北京加科思新藥研發有限公司 Ｋｒａｓ突變蛋白抑制劑
US12391692B2 (en) 2020-03-25 2025-08-19 Wigen Boimedicine Technology (Shanghai) Co., Ltd. Spiro ring-containing quinazoline compound
AU2021248363B2 (en) 2020-04-03 2024-02-15 Medshine Discovery Inc. Octahydropyrazinodiazanaphthyridine dione compounds
US20220370416A1 (en) 2020-04-06 2022-11-24 Arvinas Operations, Inc. Compounds and methods for targeted degradation of kras
WO2021203768A1 (fr) 2020-04-08 2021-10-14 江苏恒瑞医药股份有限公司 Dérivé pyrimido dicyclo, son procédé de préparation et son utilisation en médecine
CN121270550A (zh) 2020-04-16 2026-01-06 因赛特公司 稠合三环kras抑制剂
WO2021216770A1 (fr) 2020-04-22 2021-10-28 Accutar Biotechnology Inc. Composés de tétrahydroquinazoline substitués utilisés comme inhibiteurs de kras
US20230242586A1 (en) 2020-04-23 2023-08-03 The Regents Of The University Of California Ras inhibitors and uses thereof
WO2021215544A1 (fr) 2020-04-24 2021-10-28 Taiho Pharmaceutical Co., Ltd. Inhibiteurs de protéine kras g12d
EP4144732A4 (fr) 2020-04-29 2024-05-01 Shanghai Ringene BioPharma Co., Ltd. Composé de benzothiazolyle biaryle, son procédé de préparation et son utilisation
CN115151532B (zh) 2020-04-29 2023-06-06 北京泰德制药股份有限公司 喹喔啉二酮衍生物作为kras g12c突变蛋白的不可逆抑制剂
TW202144349A (zh) 2020-04-30 2021-12-01 大陸商上海科州藥物研發有限公司 作為ｋｒａｓ抑制劑的雜環化合物的製備及其應用方法
WO2021231526A1 (fr) 2020-05-13 2021-11-18 Incyte Corporation Composés de pyrimidine fusionnés utilisés comme inhibiteurs de kras
CN113666923A (zh) 2020-05-15 2021-11-19 苏州泽璟生物制药股份有限公司 烷氧基烷基取代杂环基类抑制剂及其制备方法和应用
WO2021236475A1 (fr) 2020-05-18 2021-11-25 Asinex Corporation Composés qui inhibent l'asparagine synthétase et leurs procédés d'utilisation
TWI799871B (zh) 2020-05-27 2023-04-21 大陸商勁方醫藥科技(上海)有限公司 三環并環類化合物，其製法與醫藥上的用途
CA3180314A1 (fr) 2020-05-29 2021-12-02 John Graeme HODGSON Methodes de traitement du cancer chez des patients ayant un gene kras anormal ou des deletions dans le chromosome 9
CN116034106B (zh) 2020-06-02 2025-11-04 勃林格殷格翰国际有限公司 用于治疗癌症的环状2-氨基-3-氰基噻吩及衍生物
KR20230019855A (ko) 2020-06-04 2023-02-09 안텐진 디스커버리 리미티드 Kras g12c 단백질의 억제제 및 그의 용도
WO2021245499A1 (fr) 2020-06-04 2021-12-09 Pillai Universal Llc Nouvelles petites molécules pour la dégradation ciblée de kras ne pouvant être ciblé dans une thérapie anticancéreuse
US20230026856A1 (en) 2020-06-05 2023-01-26 Sparcbio Llc Heterocyclic compounds and methods of use thereof
WO2021248079A1 (fr) 2020-06-05 2021-12-09 Sparcbio Llc Composés hétérocycliques et leurs procédés d'utilisation
WO2021248090A1 (fr) 2020-06-05 2021-12-09 Sparcbio Llc Composés hétérocycliques et leurs procédés d'utilisation
WO2021248083A1 (fr) 2020-06-05 2021-12-09 Sparcbio Llc Composés hétérocycliques et leurs procédés d'utilisation
WO2021248082A1 (fr) 2020-06-05 2021-12-09 Sparcbio Llc Composés hétérocycliques et leurs procédés d'utilisation
WO2021252339A1 (fr) 2020-06-08 2021-12-16 Accutar Biotechnology, Inc. Composés de purine -2,6-dione substitués en tant qu'inhibiteurs de kras
WO2021249563A1 (fr) 2020-06-12 2021-12-16 苏州泽璟生物制药股份有限公司 Dérivé de pyridone ou de pyrimidone aryle ou hétéroaryle, son procédé de préparation et son utilisation
US20230227466A1 (en) 2020-06-18 2023-07-20 Shy Therapeutics, Llc Substituted thienopyrimidines that interact with the ras superfamily for the treatment of cancers, inflammatory diseases, rasopathies, and fibrotic disease
WO2021259331A1 (fr) 2020-06-24 2021-12-30 南京明德新药研发有限公司 Composé hétérocyclique à huit chaînons contenant de l'azote
WO2022002102A1 (fr) 2020-06-30 2022-01-06 InventisBio Co., Ltd. Composés de quinazoline, leurs procédés de préparation et leurs utilisations
EP4182313A4 (fr) 2020-07-16 2024-10-09 Mirati Therapeutics, Inc. Inhibiteurs de kras g12d
WO2022017339A1 (fr) 2020-07-20 2022-01-27 江苏恒瑞医药股份有限公司 Dérivé pyridazinique condensé, son procédé de préparation et son utilisation pharmaceutique
WO2022028346A1 (fr) 2020-08-02 2022-02-10 上海喆邺生物科技有限公司 Composé aromatique et son application dans un médicament antitumoral
US12655160B2 (en) 2020-08-04 2026-06-16 Mirati Therapeutics, Inc. KRAS G12D inhibitors
WO2022028492A1 (fr) 2020-08-05 2022-02-10 Beigene, Ltd. Dérivés d'imidazotriazine et de pyrrolopyrimidine utilisés comme inhibiteurs de kras g12c
US20230303551A1 (en) 2020-08-13 2023-09-28 Albert Einstein College Of Medicine N-cyclyl-sulfonamides useful for inhibiting raf
EP4210833A4 (fr) * 2020-09-11 2024-09-11 Mirati Therapeutics, Inc. Formes cristallines d'un inhibiteur de kras g12c
US20230383359A1 (en) * 2020-10-23 2023-11-30 Mirati Therapeutics, Inc. Methods for treatment of lung cancers
MX2023011856A (es) * 2021-04-08 2024-01-08 Mirati Therapeutics Inc Tratamientos conjuntos que usan inhibidores de la proteína arginina n-metil transferasa 5 (prmt5) para el tratamiento de cáncer.

Also Published As

Publication number Publication date
MX2024008551A (es) 2024-07-19
EP3849538A1 (fr) 2021-07-21
AU2019340366B2 (en) 2025-01-02
US20220054491A1 (en) 2022-02-24
EP3849538A4 (fr) 2022-06-29
US20250262213A1 (en) 2025-08-21
EA202190749A1 (ru) 2021-07-09
MX2021002805A (es) 2021-07-15
KR20210075981A (ko) 2021-06-23
KR102871791B1 (ko) 2025-10-15
ZA202102015B (en) 2023-05-31
CN112955137A (zh) 2021-06-11
WO2020055756A1 (fr) 2020-03-19
AU2019340366A1 (en) 2021-04-01
IL281344A (en) 2021-04-29
IL281344B2 (en) 2025-09-01
IL281344B1 (en) 2025-05-01
JP2022500379A (ja) 2022-01-04
JP2024133474A (ja) 2024-10-02
SG11202102377YA (en) 2021-04-29
CN112955137B (zh) 2025-05-13
JP7546548B2 (ja) 2024-09-06
US12336995B2 (en) 2025-06-24

Similar Documents

Publication Publication Date Title
AU2019340366B2 (en) Combination therapies
AU2019392683B2 (en) Combination therapies
US20240408099A1 (en) COMBINATION THERAPIES OF KRAS G12D INHIBITORS WITH Pan ErbB FAMILY INHIBITORS
AU2019338207B2 (en) Combination therapies
JP7546549B2 (ja) 組み合わせ療法
EP3849537B1 (fr) Polythérapies
EP3849536A1 (fr) Polythérapies
AU2022361380A1 (en) Combination therapies of kras g12d inhibitors with sos1 inhibitors
WO2022165142A1 (fr) Polythérapies
CA3240071A1 (fr) Composes heterocycliques en tant qu'inhibiteurs de la kinase kit
EA048458B1 (ru) Способы комбинированной терапии
HK40055040A (en) Combination therapies

Legal Events

Date Code Title Description
MFA Maintenance fee for application paid

Free format text: FEE DESCRIPTION TEXT: MF (APPLICATION, 5TH ANNIV.) - STANDARD

Year of fee payment: 5

U00 Fee paid

Free format text: ST27 STATUS EVENT CODE: A-1-1-U10-U00-U101 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE REQUEST RECEIVED

Effective date: 20240730

U11 Full renewal or maintenance fee paid

Free format text: ST27 STATUS EVENT CODE: A-1-1-U10-U11-U102 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE FEE PAYMENT DETERMINED COMPLIANT

Effective date: 20240730

Free format text: ST27 STATUS EVENT CODE: A-1-1-U10-U11-U102 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE FEE PAYMENT PAID IN FULL

Effective date: 20240730

D11 Substantive examination requested

Free format text: ST27 STATUS EVENT CODE: A-1-1-D10-D11-D117 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: REQUEST FOR EXAMINATION RECEIVED

Effective date: 20240808

P11 Amendment of application requested

Free format text: ST27 STATUS EVENT CODE: A-1-1-P10-P11-P101 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: AMENDMENT RECEIVED - VOLUNTARY AMENDMENT

Effective date: 20240808

W00 Other event occurred

Free format text: ST27 STATUS EVENT CODE: A-1-1-W10-W00-W111 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: CORRESPONDENT DETERMINED COMPLIANT

Effective date: 20250311

W00 Other event occurred

Free format text: ST27 STATUS EVENT CODE: A-1-1-W10-W00-W111 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: CORRESPONDENT DETERMINED COMPLIANT

Effective date: 20250312

D00 Search and/or examination requested or commenced

Free format text: ST27 STATUS EVENT CODE: A-1-1-D10-D00-D118 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: REQUEST FOR EXAMINATION REQUIREMENTS DETERMINED COMPLIANT

Effective date: 20250317

P11 Amendment of application requested

Free format text: ST27 STATUS EVENT CODE: A-1-1-P10-P11-P102 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: AMENDMENT DETERMINED COMPLIANT

Effective date: 20250317

P13 Application amended

Free format text: ST27 STATUS EVENT CODE: A-1-1-P10-P13-X000 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: APPLICATION AMENDED

Effective date: 20250317

D11 Substantive examination requested

Free format text: ST27 STATUS EVENT CODE: A-1-2-D10-D11-D155 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: ALL REQUIREMENTS FOR EXAMINATION DETERMINED COMPLIANT

Effective date: 20250430

W00 Other event occurred

Free format text: ST27 STATUS EVENT CODE: A-2-2-W10-W00-W100 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: LETTER SENT

Effective date: 20250512

MFA Maintenance fee for application paid

Free format text: FEE DESCRIPTION TEXT: MF (APPLICATION, 6TH ANNIV.) - STANDARD

Year of fee payment: 6

U00 Fee paid

Free format text: ST27 STATUS EVENT CODE: A-2-2-U10-U00-U101 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE REQUEST RECEIVED

Effective date: 20250729

U11 Full renewal or maintenance fee paid

Free format text: ST27 STATUS EVENT CODE: A-2-2-U10-U11-U102 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE FEE PAYMENT PAID IN FULL

Effective date: 20250729

D15 Examination report completed

Free format text: ST27 STATUS EVENT CODE: A-2-2-D10-D15-D126 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: EXAMINER'S REPORT

Effective date: 20250801

P11 Amendment of application requested

Free format text: ST27 STATUS EVENT CODE: A-2-2-P10-P11-P100 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: AMENDMENT RECEIVED - RESPONSE TO EXAMINER'S REQUISITION

Effective date: 20251129

P11 Amendment of application requested

Free format text: ST27 STATUS EVENT CODE: A-2-2-P10-P11-P102 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: AMENDMENT DETERMINED COMPLIANT

Effective date: 20260109

P13 Application amended

Free format text: ST27 STATUS EVENT CODE: A-2-2-P10-P13-X000 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: APPLICATION AMENDED

Effective date: 20260109

W00 Other event occurred

Free format text: ST27 STATUS EVENT CODE: A-2-2-W10-W00-W111 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: CORRESPONDENT DETERMINED COMPLIANT

Effective date: 20260109

MFA Maintenance fee for application paid

Free format text: FEE DESCRIPTION TEXT: MF (APPLICATION, 7TH ANNIV.) - STANDARD

Year of fee payment: 7

U00 Fee paid

Free format text: ST27 STATUS EVENT CODE: A-2-2-U10-U00-U101 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE REQUEST RECEIVED

Effective date: 20260729

U11 Full renewal or maintenance fee paid

Free format text: ST27 STATUS EVENT CODE: A-2-2-U10-U11-U102 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE FEE PAYMENT PAID IN FULL

Effective date: 20260729